Design, Synthesis, and Cytotoxic Activity of New Tubulysin Analogues

Autor:	Sung Van Tran, Loc Van Tran, Hai Van Le, Chien Van Tran, Thao Thi Phuong Tran, Anh Tuan Tran
Rok vydání:	2021
Předmět:	Tetrapeptide Chemistry Organic Chemistry medicine.disease In vitro chemistry.chemical_compound Biochemistry Cell culture medicine Adenocarcinoma Cytotoxic T cell Moiety Cytotoxicity Pipecolic acid
Zdroj:	Synlett. 33:187-195
ISSN:	1437-2096 0936-5214
DOI:	10.1055/s-0041-1737139
Popis:	Synthesis of tubulysin analogues, containing an N-methyl substituent on tubuvaline-amide together with the replacement of either the hydrophobic N-terminal N-methyl pipecolic acid (Mep) or at both N- and C- terminal peptides with available heteroaromatic acids and an unsaturated tubuphenylalanine moiety, respectively, were described. The in vitro cytotoxic activity by SRB assay on five cancer cell lines for sixteen tubulysins was evaluated. Among them, five analogues exhibited strong cytotoxic activities against five human cancer cell lines, including human breast carcinoma (MCF7), human colorectal adenocarcinoma (HT-29), HL-60, SW-480, human lung adenocarcinoma (A459). Interestingly, one analogue showed the strongest cytotoxicity on all five tested cell lines even much higher toxicity than the reference compound ellipticine.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::a69a70afb6615f67caba5632bffb2f09 https://doi.org/10.1055/s-0041-1737139 Zobrazit plný text záznamu