618886-99-0Relevant articles and documents
Design, synthesis and biological activity of novel C2-C3′ N-Linked macrocyclic taxoids
Ojima, Iwao,Geng, Xudong,Lin, Songnian,Pera, Paula,Bernacki, Ralph J.
, p. 349 - 352 (2002)
A series of novel macrocyclic taxoids was designed and synthesized by connecting the C-2 and C-3′ N positions of the taxoid framework with various tethers. Cytotoxicity of these macrocyclic taxoids was evaluated against a human breast cancer cell line LCC
Design, synthesis, and biological evaluation of new-generation taxoids
Ojima, Iwao,Chen, Jin,Sun, Liang,Borella, Christopher P.,Wang, Tao,Miller, Michael L.,Lin, Songnian,Geng, Xudong,Kuznetsova, Larisa,Qu, Chuanxing,Gallager, David,Zhao, Xianrui,Zanardi, Ilaria,Xia, Shujun,Horwitz, Susan B.,Mallen-St. Clair, Jon,Guerriero, Jennifer L.,Bar-Sagi, Dafna,Veith, Jean M.,Pera, Paula,Bernacki, Ralph J.
experimental part, p. 3203 - 3221 (2009/05/11)
Novel second-generation taxoids with systematic modifications at the C2, C10, and C3′N positions were synthesized and their structure-activity relationships studied. A number of these taxoids exhibited exceptionally high potency against multidrug-resistan
Synthesis of novel C2-C3′N-linked macrocyclic taxoids by means of highly regioselective heck macrocyclization
Geng, Xudong,Miller, Michael L.,Lin, Songnian,Ojima, Iwao
, p. 3733 - 3736 (2007/10/03)
(Matrix presented) Novel C2-C3′N-linked macrocyclic taxoids are synthesized using intramolecular Heck reaction in the key step. Macrocyclization proceeds with high regioselectivity in good yield. Taxoids bearing an olefin moiety at C2 and an iodide at C3′
Synthesis and structure-activity relationships of new second-generation taxoids
Ojima, Iwao,Wang, Tao,Miller, Michael L.,Lin, Songnian,Borella, Christopher P.,Geng, Xudong,Pera, Paula,Bernacki, Ralph J.
, p. 3423 - 3428 (2007/10/03)
A series of second-generation taxoids bearing a substituent on the C-2-benzoyl group and modifications at C-3'/C-10 positions was synthesized. These taxoids exhibited 2-3 orders of magnitude higher potency than that of paclitaxel against drug-resistant human breast cancer cell lines. It is also noteworthy that three taxoids showed almost no difference in activity against drug-resistant and drug-sensitive cell lines, which are categorized as 'advanced second generation taxoids'.