In 2019,Journal of Medicinal Chemistry included an article by Lee, Taekyu; Christov, Plamen P.; Shaw, Subrata; Tarr, James C.; Zhao, Bin; Veerasamy, Nagarathanam; Jeon, Kyu Ok; Mills, Jonathan J.; Bian, Zhiguo; Sensintaffar, John L.; Arnold, Allison L.; Fogarty, Stuart A.; Perry, Evan; Ramsey, Haley E.; Cook, Rebecca S.; Hollingshead, Melinda; Davis Millin, Myrtle; Lee, Kyung-min; Koss, Brian; Budhraja, Amit; Opferman, Joseph T.; Kim, Kwangho; Arteaga, Carlos L.; Moore, William J.; Olejniczak, Edward T.; Savona, Michael R.; Fesik, Stephen W.. Application of 1129-28-8. The article was titled 《Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer》. The information in the text is summarized as follows:
Overexpression of myeloid cell leukemia-1 (Mcl-1) in cancers correlates with high tumor grade and poor survival. Addnl., Mcl-1 drives intrinsic and acquired resistance to many cancer therapeutics, including B cell lymphoma 2 family inhibitors, proteasome inhibitors, and antitubulins. Therefore, Mcl-1 inhibition could serve as a strategy to target cancers that require Mcl-1 to evade apoptosis. Herein, we describe the use of structure-based design to discover a novel compound (42) that robustly and specifically inhibits Mcl-1 in cell culture and animal xenograft models. Compound 42 binds to Mcl-1 with picomolar affinity and inhibited growth of Mcl-1-dependent tumor cell lines in the nanomolar range. Compound 42 also inhibited the growth of hematol. and triple neg. breast cancer xenografts at well-tolerated doses. These findings highlight the use of structure-based design to identify small mol. Mcl-1 inhibitors and support the use of 42 as a potential treatment strategy to block Mcl-1 activity and induce apoptosis in Mcl-1-dependent cancers. After reading the article, we found that the author used Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Application of 1129-28-8)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Application of 1129-28-8 Alkyl bromides are mainly used as alkylating agents and also find application as a solvent to extract oil from seeds and wool.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary