676627-53-5Relevant academic research and scientific papers
Synthesis of new bioisosteric hemiasterlin analogues with extremely high cytotoxicity
Anh Dang Thi, Tuyet,Pham The, Chinh,Ngo, Quoc Anh,Ha Vu Thi, Thu,Dung Nguyen, Tien,Tien Doan, Duy,Ba Thi, Cham,Jean,Van De Weghe,Nguyen Van, Tuyen
, p. 5216 - 5218 (2014)
In this Letter, the synthesis and the evaluation of the cytotoxicity of new hemiasterlin analogues were reported. The indole moiety was replaced respectively by benzofurane, naphthalene and 4-bromobenzene groups. Most of these derivatives possess strong c
Probing the interaction of HTI-286 with tubulin using a stilbene analogue
Lo, Mei-Chu,Aulabaugh, Ann,Krishnamurthy, Girija,Kaplan, Joshua,Zask, Arie,Smith, Robert P.,Ellestad, George
, p. 9898 - 9899 (2007/10/03)
HTI-286 is a synthetic analogue of the natural product hemiasterlin. HTI-286 is a potent antitumor agent that induces tubulin oligomerization. To investigate the binding stoichiometry and the binding site during this ligand-induced tubulin association, we
Synthesis and biological activity of analogues of the antimicrotubule agent N,β,β-trimethyl-L-phenylalanyl-N1-[(1S,2E)-carboxy-1- isopropylbut-2-enyl]-N13-dimethyl-L-valinamide (HTI-286)
Zask, Arie,Birnberg, Gary,Cheung, Katherine,Kaplan, Joshua,Niu, Chuan,Norton, Emily,Suayan, Ronald,Yamashita, Ayako,Cole, Derek,Tang, Zhilian,Krishnamurthy, Girija,Williamson, Robert,Khafizova, Gulnaz,Musto, Sylvia,Hernandez, Richard,Annable, Tami,Yang, Xiaoran,Discafani, Carolyn,Beyer, Carl,Greenberger, Lee M.,Loganzo, Frank,Ayral-Kaloustian, Semiramis
, p. 4774 - 4786 (2007/10/03)
Hemiasterlin (1), a tripeptide isolated from marine sponges, induces microtubule depolymerization and mitotic arrest in cells. HTI-286 (2), an analogue from an initial study of the hemiasterlins, is presently in clinical trials. In addition to its potent
