Conjugates of 17-substituted testosterone and epitestosterone with pyropheophorbide a differing in the length of linkers

Zolottsev, Vladimir A.; Ponomarev, G. V.; Taratynova, Maria O.; Morozevich, G. E.; Новиков, Роман А.; Timofeev, Vladimir P.; Solyev, Pavel N.; Zavialova, Maria G.; Zazulina, Olga V.; Tkachev, Yaroslav V.; Misharin, A. Yu.

doi:10.1016/j.steroids.2018.06.011

Cited by 5 publications

(1 citation statement)

References 31 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The results showed the hybrids’ superior cytotoxic activity compared to 5-FU, with low to moderate IC 50 values (2.39–42.21 μΜ). 17α-substituted testosterone and 17β-substituted epitestosterone conjugates with pyropheophorbide ( 32 ) through different linkers were synthesized by Zolotsev and his group, and their efficacy was investigated against two prostate cancer cell lines ( Figure 10 ) [ 83 ]. The epitestosterone conjugates were internalized more efficiently than the testosterone ones, a feature that was attributed to the structural difference between the steroidal moieties.…”

Section: Hybrids Of Natural Products With Small Moleculesmentioning

confidence: 99%

Recent Advances in Natural Product-Based Hybrids as Anti-Cancer Agents

et al. 2022

View full text Add to dashboard Cite

Cancer is one of the top leading causes of death worldwide. It is a heterogenous disease characterized by unregulated cell proliferation and invasiveness of abnormal cells. For the treatment of cancer, natural products have been widely used as a source of therapeutic ingredients since ancient times. Although natural compounds and their derivatives have demonstrated strong antitumor activity in many types of cancer, their poor pharmacokinetic properties, low cell selectivity, limited bioavailability and restricted efficacy against drug-resistant cancer cells hinder their wide clinical application. Conjugation of natural products with other bioactive molecules has given rise to a new field in drug discovery resulting to the development of novel, bifunctional and more potent drugs for cancer therapy to overcome the current drawbacks. This review discusses multiple categories of such bifunctional conjugates and highlights recent trends and advances in the development of natural product hybrids. Among them, ADCs, PDCs, ApDCs, PROTACs and AUTOTACs represent emerging therapeutic agents against cancer.

show abstract

Section: Hybrids Of Natural Products With Small Moleculesmentioning

confidence: 99%