Tag: M.W:400-500

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Horvath, Gabriela; Premkumar, Thathan; Boztas, Ali; Lee, Eunhye; Jon, Sangyong; Geckeler, Kurt E. researched the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6 ).Quality Control of cis-Dichlorobis(pyridine)platinum(II).They published the article 《Supramolecular Nanoencapsulation as a Tool: Solubilization of the Anticancer Drug trans-Dichloro(dipyridine)platinum(II) by Complexation with β-Cyclodextrin》 about this compound( cas:15227-42-6 ) in Molecular Pharmaceutics. Keywords: beta cyclodextrin trans dichlorodipyridine platinum complex nanoencapsulation solubilization anticancer. We’ll tell you more about this compound (cas:15227-42-6).

A novel, water-soluble trans-platinum complex was synthesized by inclusion complexation with β-cyclodextrin. The complexation was confirmed by 1H NMR, FT-IR, TGA, and XRD as well as by SEM and EDX. As the precursor complex is not water-soluble, it is difficult to employ it for biol. applications. Here, we report that the encapsulation with cyclodextrin allowed to solubilize the complex to a solubility value of 1.6 mg/mL. Moreover, the cytotoxicity in vitro of the novel inclusion complex indicated a much higher activity after encapsulation.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 15227-42-6, is researched, Molecular C10H10Cl2N2Pt, about The separation of nonelectrolytic geometric isomers of platinum(II) by thin-layer chromatography, the main research direction is CHROMATOG THIN LAYER; PLATINUM 2 ISOMERIC COMPLEX.Recommanded Product: 15227-42-6.

Microscope slides (75 × 25 mm.) were cleaned with detergent, rinsed in H2O, and coated with a slurry containing 1 part Silica Gel G in 3 parts of a 1:1 volume mixture of MeOH and redistilled CH2Cl2. The plates were air dried for 10-20 min. and activated for 1 hr. at 110°. Saturated solutions of the cis isomers, trans isomers, and a 1:1 by weight mixture of both Pt isomers in CH2Cl2 were applied to the plate. The plate was air dried for 2-3 min. and then developed with an ascending technique until the solvent had attained ∼6 cm. The plate was then air dried and the intense yellow-spots detected in a screw-cap jar containing I. The difference of the cis and trans migrations. ΔRf, indicated the effectiveness of separation For [Pt(Et2S)2Cl2] developed in C6H6, CH2Cl2, and 19:1 mixture of C6H6:Me2CO, ΔRf was 0.45, 0.45, and 0.45, resp. For [Pt(Bu3P)2Cl2] developed in C6H6, CH2Cl2, and a 1:1 mixture of C6H6:CH2Cl2 ΔRf was 0.95, 0.55 and 0.80, resp. For [Pt(pyridine)2Cl2] developed in CH2Cl2, 5:1 of C6H6:Me2CO Me2CO, and 5:1 of CH2Cl2:Me2CO ΔRf was 0.20, 0.45, and 0.35 resp. For [(Pr3P)2Pt2(PhS)2Cl2] developed in C6H6 and CH2Cl2 ΔRf was 0.40 and 0.45, resp. For [(Pr3P)2Pt(EtS)2Cl2] developed in CH2Cl2, 1:2 of C6H6:CH2Cl2, and C6H6 ΔRf was 0.40, 0.40, and 0.30, resp. For [Pr3P)2Pt2(p-O2NC6H4S)2Cl2] developed in CH2Cl2 and 2:1 of C6H6:Me2CO ΔRf was 0.30, 0.20, and 0.10, resp. Two (200 × 100 mm.) silica gel plates were prepared A mixture of 100 mg. cis and 100 mg. trans [Cl2Pt(PBu3)2] in CH2Cl2 were applied to the plates and developed with C6H6. The bands at Rf 0.0-0.1 and 0.85-0.10 were removed and eluted with Me2CO and CH2Cl2, resp. Evaporation yielded 91% cis isomer and 93% trans isomer. Thus, complete separation had been achieved with solvent induced isomerization.

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Tetrahydroisoquinoline – Wikipedia,
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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: cis-Dichlorobis(pyridine)platinum(II)(SMILESS: [Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2,cas:15227-42-6) is researched.Application of 693-67-4. The article 《Antitumor and antimitogenic properties of cis-dichloro(dipyridine)platinum(II)》 in relation to this compound, is published in Cancer Research. Let’s take a look at the latest research on this compound (cas:15227-42-6).

cis-Dichloro(dipyridine)platinum(II) (I) showed less potent antitumor and antimitogenic activity than previously studied cis-[Pt(NH3)2Cl2] (Rosenberg, B.; Van Camp, L., 1970). However in preliminary experiments, I was also less toxic to mice than the inorganic complex. I inhibited the growth of Escherichia coli. I increased the survival time of mice bearing Ehrlich ascites tumor; in vitro, I also inhibited protein and nucleic acid synthesis by tumors. I inhibited DNA synthesis in phytohemagglutinin-stimulated cultures of human lymphocytes.

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Tetrahydroisoquinoline – Wikipedia,
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Quality Control of cis-Dichlorobis(pyridine)platinum(II). The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: cis-Dichlorobis(pyridine)platinum(II), is researched, Molecular C10H10Cl2N2Pt, CAS is 15227-42-6, about Antitumor activity of Group VIII transition metal complexes. I. Platinum(II) complexes. Author is Cleare, Michael J.; Hoeschele, James D..

A wide variety of Pt(II) complexes were studied for antitumor activity against Sarcoma 180 in female mice. In general only neutral complexes exhibited activity, whereas charged species were inactive and relatively nontoxic. A series of complexes of the type cis-[PtA2X2] (where A2 is either 2 monodentate or 1 bidentate amine ligand and X2 is either 2 monodentate or 1 bidentate anionic ligand) were studied with A and B being systematically varied. At least 10 potentially active antitumor drugs were identified, including cis-dichlorbis(methylamine)platinum(2+) [15273-32-2], diamminepropanedioatoplatinum(2+) [38780-43-7], and (1,2-ethanediammine-N,N’)(2-methylpropanedioato)platinum(2+) [41575-97-7]. The trans isomers were inactive in comparison with active cis complexes, so the presence of cis-reactive ligands seems to be a necessary parameter for antitumor activity. Complexes with highly reactive ligands such as cis-[Pt(NH3)2 (H2O)2](NO3)2 were highly toxic. Pd(II) complexes analogous to the active Pt(II) compounds were themselves inactive.

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Tetrahydroisoquinoline – Wikipedia,
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Gale, Glen R.; Morris, Carl R.; Atkins, Loretta M.; Smith, Alayne B. published the article 《Binding of antitumor platinum compound to cells as influenced by physical factors and pharmacologically active agents》. Keywords: tumor cell platinum compound binding.They researched the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6 ).Recommanded Product: 15227-42-6. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:15227-42-6) here.

Tritiated cis-dichloro(dipyridine)platinum(II) (I) [15227-42-6] bound to intact Ehrlich ascites tumor cells at 37.deg. in vitro and remained associated with the acid-insoluble fraction of the cells. The extent of binding was also increased with increasing hydrogen ion [1333-74-0] concentration in the medium. The binding was enhanced markedly at 60.deg. and the maximum number of binding sites/cell was .sim.7 billion at this temperature Of 49 chems. and drugs tested, none decreased appreciably the rate and extent of binding, whereas certain heavy metals, and compounds that compromise membrane permeability enhanced the binding. Human and bovine lymphocytes had similar binding characteristics, but bound much more I/unit of cell volume.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 3-(2,5-Dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole(SMILESS: ClC1=NC(C2=CN(C3=C2C=CC=C3)S(=O)(=O)C2=CC=CC=C2)=C(Cl)C=N1,cas:882562-40-5) is researched.HPLC of Formula: 693-67-4. The article 《Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma》 in relation to this compound, is published in European Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:882562-40-5).

Development of inhibitors targeting CDK12/13 is of increasing interest as a potential therapy for cancers as these compounds inhibit transcription of DNA damage response (DDR) genes. We previously described THZ531, a covalent inhibitor with selectivity for CDK12/13. In order to elucidate structure-activity relationship (SAR), we have undertaken a medicinal chem. campaign and established a focused library of THZ531 analogs. Among these analogs, BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells. A 3.0 Å co-crystal structure with CDK12/CycK provides a structural rational for selective targeting of Cys1039 located in a C-terminal extension from the kinase domain. With moderate pharmacokinetic properties, BSJ-01-175 exhibits efficacy against an Ewing sarcoma tumor growth in a patient-derived xenograft (PDX) mouse model following 10 mg/kg once a day, i.p. administration. Taken together, BSJ-01-175 represents the first selective CDK12/13 covalent inhibitor with in vivo efficacy reported to date.

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Tetrahydroisoquinoline – Wikipedia,
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Norbury, A. H.; Sinha, A. I. P. published the article 《Infrared spectra (600-250cm-1) of some chloro and isocyanato complexes of palladium(II) and platinum(II)》. Keywords: palladium chloro isocyanato IR; platinum chloro isocyanato IR; isocyanato palladium platinum IR; chloro palladium platinum IR; IR palladium platinum complex.They researched the compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6 ).Recommanded Product: cis-Dichlorobis(pyridine)platinum(II). Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:15227-42-6) here.

M-NCO stretching frequencies are assigned for mixed-ligand complexes of the type ML2(NCO)2 [M = Pd(II)]. The spectra of the corresponding chloro-complexes are reported, and many of the M-Cl and M-L stretching frequencies and internal vibrations are also assigned. The geometric configurations are confirmed in most cases. The M-NCO stretching frequencies are compared with the correspondence C:N frequencies and discussed in terms of backbonding, which is particularly important for the series PdL2(NCO)2.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: cis-Dichlorobis(pyridine)platinum(II)( cas:15227-42-6 ) is researched.Related Products of 15227-42-6.Howle, Jerry A.; Gale, Glen R.; Smith, Alayne B. published the article 《Proposed mode of action of antitumor platinum compounds based upon studies with cis-dichloro([G-3H]-dipyridine)platinum(II)》 about this compound( cas:15227-42-6 ) in Biochemical Pharmacology. Keywords: chloropyridine platinum tumor; DNA dichlorodipyridine platinum; erythrocyte dichlorodipyridine platinum; RNA dichlorodipyridine platinum. Let’s learn more about this compound (cas:15227-42-6).

The antitumor and antimitotic action of the pyridine-tritiated square-planar Pt complex cis-dichloro(dipyridine)platinum(II) (I) [15227-42-6] seems to depend on the dissociation of 1 or both chlorine atoms from the platinum atom. The resulting cationic, aquated species subsequently forms a bond with nucleic acid. I associate avidly with calf thymus DNA, high mol. weight yeast RNA, and bacterial and yeast tRNA, but not with bovine serum albumin, dextran, or purified erythrocyte membranes. Dialysis of the Pt-nucleic acid complexes in distilled water or NaCl results in loss of a portion of the original radioactivity. The Pt-DNA bond is resistant to dissociation by solubilization in alkali followed by trichloroacetic acid (TCA) precipitation Bonding of I to DNA in vitro is inhibited by NaCl; however, prior alkylation of the DNA with nitrogen mustard does not influence its subsequent bonding with I. I associate with intact Ehrlich ascites tumor cells in vitro at 2.deg. and 37.deg. and resists dissociation by washing with saline or TCA as well as solubilization in alkali followed by re-precipitation with TCA.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Product Details of 882562-40-5. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 3-(2,5-Dichloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole, is researched, Molecular C18H11Cl2N3O2S, CAS is 882562-40-5, about Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Author is Kwiatkowski, Nicholas; Zhang, Tinghu; Rahl, Peter B.; Abraham, Brian J.; Reddy, Jessica; Ficarro, Scott B.; Dastur, Anahita; Amzallag, Arnaud; Ramaswamy, Sridhar; Tesar, Bethany; Jenkins, Catherine E.; Hannett, Nancy M.; McMillin, Douglas; Sanda, Takaomi; Sim, Taebo; Kim, Nam Doo; Look, Thomas; Mitsiades, Constantine S.; Weng, Andrew P.; Brown, Jennifer R.; Benes, Cyril H.; Marto, Jarrod A.; Young, Richard A.; Gray, Nathanael S..

Tumor oncogenes include transcription factors that co-opt the general transcriptional machinery to sustain the oncogenic state, but direct pharmacol. inhibition of transcription factors has so far proven difficult. However, the transcriptional machinery contains various enzymic cofactors that can be targeted for the development of new therapeutic candidates, including cyclin-dependent kinases (CDKs). Here the authors present the discovery and characterization of a covalent CDK7 inhibitor, THZ1, which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. Cancer cell-line profiling indicates that a subset of cancer cell lines, including human T-cell acute lymphoblastic leukemia (T-ALL), have exceptional sensitivity to THZ1. Genome-wide anal. in Jurkat T-ALL cells shows that THZ1 disproportionally affects transcription of RUNX1 and suggests that sensitivity to THZ1 may be due to vulnerability conferred by the RUNX1 super-enhancer and the key role of RUNX1 in the core transcriptional regulatory circuitry of these tumor cells. Pharmacol. modulation of CDK7 kinase activity may thus provide an approach to identify and treat tumor types that are dependent on transcription for maintenance of the oncogenic state.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: cis-Dichlorobis(pyridine)platinum(II)(SMILESS: [Cl-][Pt+2]([N]1=CC=CC=C1)([Cl-])[N]2=CC=CC=C2,cas:15227-42-6) is researched.Related Products of 1452-77-3. The article 《Experimental and theoretical study of the cytotoxic activity of new tetrazole-containing cisplatin analogues and their trans-isomers》 in relation to this compound, is published in Doklady Natsional’noi Akademii Nauk Belarusi. Let’s take a look at the latest research on this compound (cas:15227-42-6).

Quantum chem. calculations within the framework of DFT were carried out for a set of platinum (II) complexes with nitrogen-containing heterocycles. A phys. interpretable QSAR model was developed and a correlation between the biol. activity and structural properties was obtained by means of the multiple linear regression method. The range of new tetrazole-containing platinum (II) complexes was synthesized, and their cytotoxic activity was exptl. determined and compared with the values predicted by the QSAR model. Crucial properties of compounds and their relationship with the mode of action were discussed.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem