- 1-(3,4,5-Trimethoxyphenyl)ethane-1,2-diyl esters, a novel compound class with potent chemoreversal activity
-
1-(3,4,5-Trimethoxyphenyl)ethane-1,2-diyl esters, which share a fragment from (±)-3′-O-4′-O-bis(3,4-dimethoxycinnamoyl)-cis- khellactone (DMDCK) and 3′R,4′R-disubstituted-2′,2′- dimethyldihydropyrano[2,3-f]chromone (DSP), exhibited remarkable chemoreversa
- Hung, Hsin-Yi,Ohkoshi, Emika,Goto, Masuo,Nakagawa-Goto, Kyoko,Lee, Kuo-Hsiung
-
p. 7726 - 7729
(2013/02/23)
-
- CN-assisted oxidative cyclization of cyano cinnamates and styrene derivatives: A facile entry to 3-substituted chiral phthalides
-
The asymmetric dihydroxylation (AD) of o-cyano cinnamates and styrene derivatives leads to efficient construction of chiral phthalide frameworks in high optical purities. This unique reaction is characterized by unusual synergism between CN and osmate groups resulting in rate enhancement of the AD process. The method is amply demonstrated by the synthesis and the structural/stereochemical assignment of the natural products.
- Reddy, R.Santhosh,Kiran, I. N. Chaithanya,Sudalai, Arumugam
-
scheme or table
p. 3655 - 3661
(2012/05/31)
-
- New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models
-
During a screen for compounds that could inhibit cell proliferation, a series of new tubulin-binding compounds was identified with the discovery of oxadiazoline 1 (A-105972). This compound showed good cytotoxic activity against non-multi-drug-resistant and multi-drug-resistant cancer cell lines, but its utility in vivo was limited by a short half-life. Medicinal chemistry efforts led to the discovery of indolyloxazoline 22g (A-259745), which maintained all of the in vitro activity seen with oxadiazoline 1, but also demonstrated a better pharmacokinetic profile, and dose-dependent in vivo activity. Over a 28 day study, indolyloxazoline 22g increased the life span of tumor-implanted mice by up to a factor of 3 upon oral dosing. This compound, and others of its structural class, may prove to be useful in the development of new chemotherapeutic agents to treat human cancers.
- Szczepankiewicz,Chiou,Credo,Alder,Nukkala,Zielinski,Jarvis,Mollison,Frost,Bauch,Hui,Liu,Claiborne,Li,Rosenberg,Jae,Tasker,Gunawardana,Von Geldern,Gwaltney II,Wu-Wong,Gehrke
-
p. 4416 - 4430
(2007/10/03)
-