78502-71-3Relevant articles and documents
Design, synthesis, and antitumor activity evaluation of pretubulysin analogs
Xu, Xiangrong,Fan, Meixia,Qi, Junhui,Yao, Lei
, p. 341 - 351 (2021/06/14)
Pretubulysin, a biosynthetic precursor of the tubulysins, shows potent biological activity in a variety of tumor cell lines. Although there are several total synthesis routes to tubulysin and pretubulysin reported, the commercialization still has been hampered due to the complexity of the structure. To find structurally simpler pretubulysin analogs, a series of 2-(3-(methylamino)propyl)thiazole-4-carboxamides are designed and synthesized, and their anticancer activities are screened using MCF-7 (breast cancer), and NCI-H157 (lung cancer) cell lines. Taxol (IC50?=?0.01?μM) and pretubulysin are used as the control. Compounds 8c (IC50?=?0.05?μM, MCF-7; 0.09?μM, NCI-H157) and 8h (IC50?=?0.01?μM, MCF-7; 0.02?μM, NCI-H157) exhibited certain antitumor activities comparable to those of Taxol. The urea analogs of pretubulysin might represent a promising scaffold for the further development of novel antitumor drugs.
Sulfur-containing compound based on glutaryl imide skeleton and application of compound
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Paragraph 0763-0764, (2020/09/12)
The present disclosure relates to compound shown in a formula (I) or salts, solvates, isotope-enriched analogs, tautomers, polymorphs, stereoisomers, or mixtures of stereoisomers of the compound, andthe application thereof in the treatment of tumours. The present disclosure also provides tumor treatment application of the compound showed in a formula (I') or pharmaceutically acceptable salts, solvates, isotope-enriched analogs, tautomers, polymorphic substances, stereoisomers, or mixtures of stereoisomers of the compound.
NEW BRADYKININ B1 ANTAGONISTS
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Page/Page column 156, (2010/04/03)
The invention relates to compounds of formula (I) where in R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.