1219930-75-2Relevant academic research and scientific papers
TUBULYSIN ANALOGUES AS ANTICANCER AGENTS AND PAYLOADS FOR ANTIBODY-DRUG CONJUGATES AND METHODS OF TREATMENT THEREWITH
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Page/Page column 59-60, (2019/06/17)
In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect
Improved Total Synthesis of Tubulysins and Design, Synthesis, and Biological Evaluation of New Tubulysins with Highly Potent Cytotoxicities against Cancer Cells as Potential Payloads for Antibody-Drug Conjugates
Nicolaou,Erande, Rohan D.,Yin, Jun,Vourloumis, Dionisios,Aujay, Monette,Sandoval, Joseph,Munneke, Stefan,Gavrilyuk, Julia
, p. 3690 - 3711 (2018/03/21)
Improved, streamlined total syntheses of natural tubulysins such as V (Tb45) and U (Tb46) and pretubulysin D (PTb-D43), and their application to the synthesis of designed tubulysin analogues (Tb44, PTb-D42, PTb-D47-PTb-D49, and Tb50-Tb120), are described.
Total Synthesis and Biological Evaluation of Natural and Designed Tubulysins
Nicolaou,Yin, Jun,Mandal, Debashis,Erande, Rohan D.,Klahn, Philipp,Jin, Michael,Aujay, Monette,Sandoval, Joseph,Gavrilyuk, Julia,Vourloumis, Dionisios
, p. 1698 - 1708 (2016/02/20)
A streamlined total synthesis of N14-desacetoxytubulysin H (Tb1) based on a C-H activation strategy and a short total synthesis of pretubulysin D (PTb-D43) are described. Applications of the developed synthetic strategies and technologies to the synthesis of a series of tubulysin analogues (Tb2-Tb41 and PTb-D42) are also reported. Biological evaluation of the synthesized compounds against an array of cancer cells revealed a number of novel analogues (e.g., Tb14), some with exceptional potencies against certain cell lines [e.g., Tb32 with IC50 = 12 pM against MES SA (uterine sarcoma) cell line and 2 pM against HEK 293T (human embryonic kidney) cell line], and a set of valuable structure-activity relationships. The highly potent cytotoxic compounds discovered in this study are highly desirable as payloads for antibody-drug conjugates and other drug delivery systems for personalized targeted cancer chemotherapies.
DESACETOXYTUBULYSIN H AND ANALOGS THEREOF
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, (2016/09/22)
In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein R1, R2, R3, R4, X1, X2, X3, and A1 are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein.
BIOACTIVE PRE-TUBULYSINS AND USE THEREOF
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, (2011/10/13)
The invention relates to bioactive pre-tubulysin derivatives, their preparation and pharmacological use.
Synthesis and biological evaluation of pretubulysin and derivatives
Ullrich, Angelika,Herrmann, Jennifer,Mueller, Rolf,Kazmaier, Uli
experimental part, p. 6367 - 6378 (2011/03/21)
Pretubulysin, a biosynthetic precursor of the tubulysins, shows potent biological activity in the subnanomolar range towards various tumor cell lines. Its activity is only slightly less than those of the structurally more complex tubulysins. With a straig
