937271-43-7Relevant articles and documents
Homogeneous and Functional Group Tolerant Ring-Closing Metathesis for DNA-Encoded Chemical Libraries
Monty, Olivier B. C.,Nyshadham, Pranavanand,Bohren, Kurt M.,Palaniappan, Murugesan,Matzuk, Martin M.,Young, Damian W.,Simmons, Nicholas
, p. 80 - 88 (2020)
Reaction heterogeneity, poor pH control, and catalyst decomposition in the ring-closing metathesis (RCM) of DNA-chemical conjugates lead to poor yields of the cyclized products. Herein we address these issues with a RCM reaction system that includes a novel aqueous solvent combination to enable reaction homogeneity, an acidic buffer system which masks traditionally problematic functional groups, and a decomposition-resistant catalyst which maximizes conversion to the cyclized product. Additionally, we provide a systematic study of the substrate scope of the on-DNA RCM reaction, a demonstration of its applicability to a single-substrate DNA-encoded chemical library that includes sequencing analysis, and the first successful stapling of an unprotected on-DNA [i, i+4] peptide.
COVALENT INHIBITORS OF CDK-7
-
Page/Page column 59-60, (2016/10/04)
This disclosure includes compounds of Formula (I), wherein A, B, C, R1, R2, R3, R5, R6, m, n, W1, W2, Z1, Z2, Z3, Z4, L1, L2, and warhead are defined herein. Also disclosed is a method for treating a neoplastic disease with these compounds.
Macrocyclic compounds as anti-cancer agents: Design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2
Ning, Cheng-Qing,Lu, Cheng,Hu, Liang,Bi, Yan-Jing,Yao, Lei,He, Yu-Jun,Liu, Li-Fei,Liu, Xiao-Yu,Yu, Nie-Fang
, p. 104 - 115 (2015/03/30)
A novel series of macrocyclic compounds were designed and synthesized as multi-target inhibitors targeting HDAC, FLT3 and JAK2. Some of these compounds exhibited potent HDAC inhibition as well as FLT3 and JAK2 inhibition under both cell-free and cellular conditions. In vitro antiproliferative assay indicated that these compounds were interestingly more cytotoxic to MV4-11 cells bearing FLT3-ITD mutation and HEL cells bearing JAK2V617F mutation.