207910-90-5Relevant articles and documents
IMMUNOMODULATOR ANTIBODY DRUG CONJUGATES AND USES THEREOF
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Paragraph 00529-00530; 00558-00559, (2020/12/30)
Provided herein are compounds, trifunctional antibody products thereof, and methods and pharmaceutical compositions for use in treatment of inflammatory and/or proliferative diseases.
Carbonic Anhydrase XII Inhibitors Overcome Temozolomide Resistance in Glioblastoma
Mujumdar, Prashant,Kopecka, Joanna,Bua, Silvia,Supuran, Claudiu T.,Riganti, Chiara,Poulsen, Sally-Ann
, p. 4174 - 4192 (2019/05/01)
The natural product primary sulfonamide, psammaplin C (1), when used in combination with clinically used chemotherapeutic drugs, including temozolomide, reverses multidrug resistance and increases survival in glioblastoma, a highly aggressive primary brain tumor. We showed previously that the mechanism of action of 1 is novel, acting to indirectly interfere with P-glycoprotein drug efflux activity as a consequence of carbonic anhydrase XII (CA XII) inhibition. To build structure-activity relationships, 45 derivatives of 1 were designed, synthesized, and evaluated against a panel of CA isoforms. Compound 55 was identified as a potent inhibitor of CA XII (Ki = 0.56 nM) and was investigated in vitro and in vivo using samples from glioblastoma patients. The results strengthen the possibility that co-therapy of temozolomide with a CA XII inhibitor may more effectively treat glioblastoma by suppressing an important temozolomide resistance mechanism.
HEMIASTERLIN DERIVATIVES FOR CONJUGATION AND THERAPY
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Paragraph 00290-00291, (2016/08/23)
Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000: or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W1, W4, W5, SG, and R are as described herein.
Synthesis and activity of novel analogs of hemiasterlin as inhibitors of tubulin polymerization: Modification of the a segment
Yamashita, Ayako,Norton, Emily B.,Kaplan, Joshua A.,Niu, Chuan,Loganzo, Frank,Hernandez, Richard,Beyer, Carl F.,Annable, Tami,Musto, Sylvia,Discafani, Carolyn,Zask, Arie,Ayral-Kaloustian, Semiramis
, p. 5317 - 5322 (2007/10/03)
Analogs of HTI-286 (1), containing various aromatic rings in the A segment, were synthesized as potential inhibitors of tubulin polymerization, and the structure-activity relationships related to stereo- and regio-chemical effects of substituents on the a
