54253-05-3Relevant articles and documents
Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT)
Hwang, Jong Yeon,Smithson, David,Zhu, Fangyi,Holbrook, Gloria,Connelly, Michele C.,Kaiser, Marcel,Brun, Reto,Guy, R. Kiplin
, p. 2850 - 2860 (2013/05/21)
We previously reported the discovery of the activity of chloronitrobenzamides (CNBs) against bloodstream forms of Trypanosoma brucei. Herein we disclose extensive structure-activity relationship and structure-property relationship studies aimed at identification of tractable early leads for clinical development. These studies revealed a promising lead compound, 17b, that exhibited nanomolar potency against T. brucei (EC 50 = 27 nM for T. b. brucei, 7 nM for T. b. rhodesiense, and 2 nM for T. b. gambiense) with excellent selectivity for parasite cells relative to mammalian cell lines (EC50 > 25 μM). In addition compound 17b displayed suitable physiochemical characteristics and microsomal stability (t1/2 > 4 h for human and mouse) to justify pursuing in vivo studies.
Synthesis and antitumor activity of novel benzophenone derivatives
Kumazawa, Eiji,Hirotani, Kenji,Burford, S. Clifford,Kawagoe, Keiichi,Miwa, Tamotsu,Mitsui, Ikuo,Ejima, Akio
, p. 1470 - 1474 (2007/10/03)
Novel benzophenone derivatives were synthesized and screened for cytotoxic and antitumor activity. Friedel-Crafts condensation was employed to construct the benzophenone skeleton. Among the compounds synthesized, morpholino and thiomorpholino benzophenones 3a-d exhibited potent cytotoxic activity against P388 murine leukemia and PC-6 human lung carcinoma cells in vitro, and compounds 3a, 3c, and 3j, when administered intraperitoneally, showed significant antitumor activity against the malignant ascites caused by intraperitoneal inoculation of P388 cells in mice.