Diaza- and triazachrysenes: potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435
摘要:
Several 5,12-diazachrysen-6-ones and 5,6,11-triazachrysen-12-ones were synthesized with varied substituents at the 5- or 11-position, respectively. Each compound was evaluated for its potential to stabilize the cleavable complex formed with TOP I and DNA. Two analogues with very potent TOP1-targeting activity, 3a and 4a, exhibited cytotoxic activity with IC50 values at or below 2 nM against RPM18402. Compound 3a was active in vivo by either ip or po administration in the human tumor xenograft athymic nude mice model. (C) 2002 Elsevier Science Ltd. All rights reserved.
Aminoalkylthiopyranopyrroles and related compounds of the formula ##SPC1## In which R.sub.1, R.sub.2, R.sub.3, X, m, n and p are as defined below, and their physiologically tolerable acid addition salts are disclosed to possess antiinflammatory and antiarrhythmic properties. A process for their preparation is also disclosed.
Aminoalkylthiopyranopyrroles及相关化合物的化学式如下所示:##SPC1## 其中R.sub.1, R.sub.2, R.sub.3, X, m, n和p的定义如下,并且其生理耐受性酸盐被披露具有抗炎和抗心律失常的特性。同时还披露了它们的制备方法。
[EN] NOVEL DIHYDROQUINOLIZINONES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION<br/>[FR] NOUVELLES DIHYDROQUINOLIZINONES POUR LE TRAITEMENT ET LA PROPHYLAXIE D'UNE INFECTION PAR LE VIRUS DE L'HÉPATITE B
申请人:HOFFMANN LA ROCHE
公开号:WO2015173164A1
公开(公告)日:2015-11-19
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R6, X and Y are as described in the description and in the claims, as well as or pharmaceutically acceptable salts, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
Compounds and methods for inhibiting the interaction of BCL proteins with binding partners
申请人:Castro C. Alfredo
公开号:US20060025460A1
公开(公告)日:2006-02-02
One aspect of the present invention relates to heterocyclic compounds that bind to bcl proteins and inhibit Bcl function. Another aspect of the present invention relates to compositions comprising a heterocyclic compound of the invention. The present invention provides methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
本发明涉及有机分子,能够调节酪氨酸激酶信号传导,以调节、调控和/或抑制异常细胞增殖。
Development of broad-spectrum enterovirus antivirals based on quinoline scaffold
作者:Rami Musharrafieh、Naoya Kitamura、Yanmei Hu、Jun Wang
DOI:10.1016/j.bioorg.2020.103981
日期:2020.8
developing potent and broad-spectrum antiviralsagainst these non-polio enteroviruses. Starting from our previously developed lead compounds that had potent antiviral activity against EV-D68, we synthesized 43 analogs and profiled their broad-spectrum antiviral activity against additional EV-D68, EV-A71, and CVB3 viruses. Promising candidates were also selected for mouse microsomal stability test to prioritize