Chang C.-I.,National Pingtung University of Science and Technology |
Li Y.-C.,National Taiwan University |
Yang C.-S.,China Medical University at Taichung |
Chao C.-Y.,Asia University, Taiwan |
And 7 more authors.
Helvetica Chimica Acta | Year: 2015
Two new labdane-type diterpene acids, (12S)-12-hydroxylabda-8(17),13(16),14-trien-18-oic acid (1) and (12R)-12-hydroxy-15,16-epoxylabda-8(17),13-dien-18-oic acid (2), along with a known labdane-type diterpene, (11E)-15,16-bisnor-13-oxolabda-8(17),11-dien-19-oic acid (3), were isolated from the MeOH extract of the wood of Cunninghamia konishii. Their structures were determined by analysis of spectroscopic data and comparison with the data of known analogs. © 2015 Verlag Helvetica Chimica Acta AG, Zürich. Source
Design and synthesis of tetrahydropyridothieno[2,3-d]pyrimidine scaffold based epidermal growth factor receptor (EGFR) kinase inhibitors: The role of side chain chirality and michael acceptor group for maximal potency
Wu C.-H.,Institute of Biotechnology and Pharmaceutical Research |
Wu C.-H.,National Tsing Hua University |
Coumar M.S.,Institute of Biotechnology and Pharmaceutical Research |
Chu C.-Y.,Institute of Biotechnology and Pharmaceutical Research |
And 22 more authors.
Journal of Medicinal Chemistry | Year: 2010
HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 antiproliferative activity compared to HTS hit 7 and also inhibited gefitinib-resistant double mutant (DM, T790M/L858R) EGFR kinase at nanomolar concentration. Moreover, treatment with 19 shrinked tumor in nude mice xenograft model. © 2010 American Chemical Society. Source