Design, synthesis, and biological activity evaluation of campthothecin‐HAA‐Norcantharidin conjugates as antitumor agents in vitro

  title={Design, synthesis, and biological activity evaluation of campthothecin‐HAA‐Norcantharidin conjugates as antitumor agents in vitro},
  author={Xian H Wang and Mei-Hui Huang and Changkuo Zhao and Chan Li and Lang Xu},
  journal={Chemical Biology \& Drug Design},
  pages={986 - 992}
Three components of Camptothecin, hydroxyacetic acid, and functionalized norcantharidins were constructed together to form a novel series of camptothecin derivatives in a good yield. The synthesized campthothecin‐HAA‐norcantharidin conjugate pro‐drugs could suppress cancer cell growth in vitro. These conjugated pro‐drug molecules possess therapeutic potential as novel bi‐functional conjugates platforms for cancer treatment. 

Synthesis of l-ascorbic acid-amino acid-norcantharidin conjugates and their biological activity evaluation in vitro.

The results showed that compounds 6e, 6g, 6j, 6l, 6m, 6b, 6 e, 6i, and 6n showed high cytotoxicity to HepG2 and compounds 6 b, 6e-g, 7b, 7d, 7h, 7i, 7n, 8g, 8i exhibited high cytOToxicity to SW480.

Targeting Production of Reactive Oxygen Species as an Anticancer Strategy

The difference in cellular redox balance between normal and cancer cells is discussed as a potential anticancer target, along with various examples of approved or experimental drugs that may alter the redox state, and drugs are presented in relation to their pro-oxidant or antioxidant mechanisms.

Suitability of Ferrites for Biomedical Applications

This chapter aims at the latest amelioration in the biomedical application of spinel ferrites, which has many benefits over traditional methods used for disease diagnosis and imaging treatment of chronic carcinogenic origin diseases.



Sealed tube promoted coupling of camptothecin and norcantharidin acid ester and their preliminary biological activity evaluation in vitro

A facile synthetic method was developed for the novel acid-sensitive camptothecin norcantharidin acid ester derivatives 3 in sealed tube which shows better activity against several tumor cell lines in vitro test.

A series of alpha-amino acid ester prodrugs of camptothecin: in vitro hydrolysis and A549 human lung carcinoma cell cytotoxicity.

Results suggest that 2d is the best candidate for a passively targeted sustained release lung delivery system, indicating a higher cell death rate at lower concentrations than CPT and the other prodrugs tested.

Rational design of multifunctional small-molecule prodrugs for simultaneous suppression of cancer cell growth and metastasis in vitro and in vivo.

These "all-in-one" prodrug constructs possess therapeutic potential as novel "integrative" platforms for metastatic cancer treatment and are presented as design concept for multifunctional prodrugs that simultaneously induce apoptosis and suppress cancer cell metastasis in vitro and in vivo.

QSAR, docking and ADMET studies of camptothecin derivatives as inhibitors of DNA topoisomerase‐I

The quantitative structure–activity relationship (QSAR) models of camptothecin derivatives against DNA Topoisomerase‐I (DNA Topo‐I) were developed by multiple linear regression method using leave‐one‐out validation approach and indicates that chemical descriptors are correlated well with activity.

A new strategy to improve the metabolic stability of lactone: discovery of (20S,21S)-21-fluorocamptothecins as novel, hydrolytically stable topoisomerase I inhibitors.

Results revealed that the conserved C21-carbonyl group of camptothecin can be replaced by a fluorine substituent, which indicates that α-Fluoro ether may have general application in improving the metabolic stability of lactone.

Supramolecular "Trojan Horse" for Nuclear Delivery of Dual Anticancer Drugs.

A simple strategy to construct supramolecular nanomedicines for nuclear delivery of dual synergistic anticancer drugs using the coassembly of a negatively charged HCPT-peptide amphiphile and the positively charged cisplatin to promote the synergistic tumor suppression property in vivo.

HPMA copolymer bound adriamycin overcomes MDR1 gene encoded resistance in a human ovarian carcinoma cell line.