125791-83-5Relevant articles and documents
LIPID DERIVATIVES FOR IN VITRO OR IN VIVO DELIVERY
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Page/Page column 59, (2019/07/13)
The present invention relates to novel constructs that allow for delivery of biologically active agents into cells. In certain embodiments, the constructs comprises conjugates of a lipophilic membrane dye, or a derivative or analogue thereof, with the biologically active agent.
ABIRATERONE DERIVATIVES AND NON-COVALENT COMPLEXES WITH ALBUMIN
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Page/Page column 63-65, (2016/01/12)
The present disclosure provides derivatives of abiraterone, non-covalently bound complexes of the abiraterone derivatives with serum albumin, pharmaceutical compositions of the same, and methods of use thereof. The non-covalently bound complexes are significantly more water-soluble than abiraterone and are useful for the treatment of a disease or condition that can benefit from CYP17 inhibition, such as prostate cancer.
Design, synthesis, and biological evaluations of tumor-targeting dual-warhead conjugates for a taxoid-camptothecin combination chemotherapy
Vineberg, Jacob G.,Zuniga, Edison S.,Kamath, Anushree,Chen, Ying-Jen,Seitz, Joshua D.,Ojima, Iwao
, p. 5777 - 5791 (2014/08/05)
Novel tumor-targeting dual-warhead conjugates, 2 (DW-1) and 3 (DW-2), which consist of a next-generation taxoid, 1 (SB-T-1214), and camptothecin as two warheads, self-immolative disulfide linkers for drug release, biotin as the tumor-targeting moiety, and 1,3,5-triazine as the tripod splitter module, were designed and synthesized. The potency of 2 was evaluated against MX-1, MCF-7, ID8, L1210FR (BR+, biotin receptor overexpressed) and WI38 (BR-, normal) cell lines in the absence and presence of glutathione (GSH), which is an endogenous thiol that triggers drug release inside the cancer cells. With the GSH and resuspension protocol, 2 exhibited IC50 values of 3.22-9.80 nM against all BR+ cancer cell lines, and 705 nM against WI38. Thus, there was a two orders of magnitude higher selectivity to cancer cells. Also, a clear cooperative effect was observed for the taxoid-camptothecin combination when two drugs were delivered to the cancer cells specifically in the form of a dual-warhead conjugate.