13991-36-1Relevant articles and documents
Development of resin-to-resin transfer reactions (RRTR) using Sonogashira chemistry
Tulla-Puche, Judit,Barany, George
, p. 2195 - 2201 (2005)
Sonogashira chemistry can be used according to the 'resin-to-resin transfer reaction' (RRTR) concept. Two fragments, one containing the halide moiety and the second one incorporating the alkyne functionality, are anchored on different solid supports using
Biosynthesis of salinosporamides from α,β-unsaturated fatty acids: Implications for extending polyketide synthase diversity
Liu, Yuan,Hazzard, Christopher,Eustaquio, Alessandra S.,Reynolds, Kevin A.,Moore, Bradley S.
, p. 10376 - 10377 (2009)
(Chemical Equation Presented) A new series of coenzyme A-tethered polyketide synthase extender units were discovered in relation to the biosynthesis of the salinosporamide family of anticancer agents from the marine bacterium Salinispora tropica. In vivo and in vitro experiments revealed that the crotonyl-CoA reductase/carboxylase SalG has broad substrate tolerance toward 2-alkenyl-CoAs that give rise to the salinosporamide C-2 substitution pattern.
Design and synthesis of novel benzothiophene analogs as selective estrogen receptor covalent antagonists against breast cancer
Bai, Chengfeng,Ren, Shengnan,Wu, Shuangjie,Zhu, Meiqi,Luo, Guoshun,Xiang, Hua
, (2021/05/27)
Endocrine therapy (ET) has benefited patients with estrogen receptor alpha (ERα) positive breast cancer for decades. Selective estrogen receptor modulator (SERM) such as Tamoxifen represents the clinical standard of care (SoC). Despite the therapeutic importance of current SoC agents, 30–50% of prolonged treatment patients inevitably generated resistant tumor cells, usually eventually suffered tumor relapse and developed into metastatic breast cancer (MBC), which was the leading cause of female cancer-related mortality. Among these, most resistant tumors remained dependent on ERα signaling, which reignited the need for the next generation of ERα related agents. We hypothesized that selective estrogen receptor covalent antagonists targeting ERα would provide a therapeutic alternative. In the current work, series of novel benzothiophene hybrids bearing electrophile moieties were synthesized and biologically evaluated. The representative analogue 15c exhibited potent anti-proliferative effect in MCF-7 cell lines in vitro, and further mechanism studies confirmed the necessity of covalent bonding. More importantly, 15c could attenuate the expression of TFF-1, GREB-1 and downregulate the levels of cellular ERα protein.
SUMO INHIBITOR COMPOUNDS AND USES THEREOF
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Paragraph 0187, (2020/10/09)
The present invention relates to compounds and compositions capable of acting as inhibitors of small ubiquitin-like modifier (SUMO) family of proteins. The compounds and compositions may be used in the treatment of cancer. There are disclosed, inter alia, methods of inhibiting an E1 enzyme, and compounds useful for inhibiting an E1 enzyme.
ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
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Paragraph 0181; 0182; 0183, (2019/07/23)
The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description.
