TY  - JOUR
AB  - Traditional chemotherapeutics used in cancer therapy do not preferentially accumulate in tumor tissues. The conjugation to delivery vehicles like antibodies or small molecules has been proposed as a strategy to increase the tumor uptake and improve the therapeutic window of these drugs. Here, we report the synthesis and the biological evaluation of a novel small molecule-drug conjugate (SMDC) comprising a high-affinity bidentate acetazolamide derivative, targeting carbonic anhydrase IX (CAIX), and cryptophycin, a potent microtubule destabilizer. The biological activity of the novel SMDC was evaluated in vitro, measuring binding to the CAIX antigen by surface plasmon resonance and cytotoxicity against SKRC-52 cells. In vivo studies showed a delayed growth of tumors in nude mice bearing SKRC-52 renal cell carcinomas.
DA  - 2018
DO  - 10.1021/acsomega.8b02350
LA  - eng
IS  - 11
M2  - 14726
PY  - 2018
SN  - 2470-1343
SP  - 14726-14731
T2  - ACS Omega
TI  - In Vivo Antitumor Activity of a Novel Acetazolamide-Cryptophycin Conjugate for the Treatment of Renal Cell Carcinomas
UR  - https://nbn-resolving.org/urn:nbn:de:0070-pub-29329842
Y2  - 2024-11-22T04:55:36
ER  -