Semi-synthesis and biological activity of γ-lactones analogs of camptothecin

Li, Mingzong; Tang, Weidong; Zeng, Fuxing; Lou, Liguang; You, Tianyan

doi:10.1016/j.bmcl.2008.10.074

Cited by 13 publications

(7 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…With IC 50 values of 1.28 and 2.03 μM against A549 and HT‐29 cancer cell lines, only compound 164 (Fig. ) showed cytotoxic activity similar to TPT ( 3 ) …”

Section: Biological Activity Of Cpt and Related Derivativesmentioning

confidence: 99%

“…22) showed cytotoxic activity similar to TPT (3). 80 Recently, due to the important role of fluorine substitution in drug design, a series of (20S,21S)-21-fluorocamptothecins was designed and synthesized. All of these analogs showed potent in vitro antitumor activities and were potent topo I inhibitors with increased hydrolytic stability.…”

Section: A B and E Ring Modified Cpt Analogsmentioning

confidence: 99%

See 1 more Smart Citation

Perspectives on Biologically Active Camptothecin Derivatives

et al. 2015

View full text Add to dashboard Cite

Camptothecins (CPTs) are cytotoxic natural alkaloids that specifically target DNA topoisomerase I. Research on CPTs has undergone a significant evolution from the initial discovery of CPT in the late 1960s through the study of synthetic small molecule derivatives to investigation of macromolecular constructs and formulations. Over the past years, intensive medicinal chemistry efforts have generated numerous CPT derivatives. Three derivatives, topotecan, irinotecan, and belotecan, are currently prescribed as anticancer drugs, and several related compounds are now in clinical trials. Interest in other biological effects, besides anticancer activity, of CPTs is also growing exponentially, as indicated by the large number of publications on the subject during the last decades. Therefore, the main focus of the present review is to provide an ample but condensed overview on various biological activities of CPT derivatives, in addition to continued up-to-date coverage of anticancer effects.

show abstract

“…With IC 50 values of 1.28 and 2.03 μM against A549 and HT‐29 cancer cell lines, only compound 164 (Fig. ) showed cytotoxic activity similar to TPT ( 3 ) …”

Section: Biological Activity Of Cpt and Related Derivativesmentioning

confidence: 99%

Section: A B and E Ring Modified Cpt Analogsmentioning

confidence: 99%

Perspectives on Biologically Active Camptothecin Derivatives

et al. 2015

View full text Add to dashboard Cite

show abstract

“…Camptothecin (CPT) is a major anti-cancer drug that shows efficacy toward many cancers, including ovarian and colorectal tumours. CPT is an alkaloid isolated in the early 1960s from the Chinese tree, Camptotheca acuminata 7 . CPT is a selective topoisomerase I inhibitor 8 .…”

Section: Introductionmentioning

confidence: 99%

Efficiency of newly formulated camptothecin with β-cyclodextrin-EDTA-Fe3O4 nanoparticle-conjugated nanocarriers as an anti-colon cancer (HT29) drug

Krishnan

Rajan

Kumari

et al. 2017

Sci Rep

View full text Add to dashboard Cite

Camptothecin (CPT) is an anti-cancer drug that effectively treats various cancers, including colon cancer. However, poor solubility and other drawbacks have restricted its chemotherapeutic potential. To overcome these restrictions, CPT was encapsulated in CEF (cyclodextrin-EDTA-FE3O4), a composite nanoparticle of magnetic iron oxide (Fe3O4), and β-cyclodextrin was cross-linked with ethylenediaminetetraacetic acid (EDTA). This formulation improved CPT’s solubility and bioavailability for cancer cells. The use of magnetically responsive anti-cancer formulation is highly advantageous in cancer chemotherapy. The chemical characterisation of CPT-CEF was studied here. The ability of this nano-compound to induce apoptosis in HT29 colon cancer cells and A549 lung cancer cells was evaluated. The dose-dependent cytotoxicity of CPT-CEF was shown using MTT. Propidium iodide and Annexin V staining, mitochondrial membrane depolarisation (JC-1 dye), and caspase-3 activity were assayed to detect apoptosis in CPT-CEF-treated cancer cells. Cell cycle analysis also showed G1 phase arrest, which indicated possible synergistic effects of the nano-carrier. These study results show that CPT-CEF causes a dose-dependent cell viability reduction in HT29 and A549 cells and induces apoptosis in colon cancer cells via caspase-3 activation. These data strongly suggest that CPT could be used as a major nanocarrier for CPT to effectively treat colon cancer.

show abstract

“…The alkaloid compound of CPT was initially isolated from a Chinese tree, Camptotheca acumincta, in the early 1960s. 26 CPT is recognized as a selective topoisomerase I inhibitor. 27 Emerging studies proposed that the potential of CPT to act as anti-tumor agent might be attributed to its ability to inhibit nitric oxide (NO) biosynthesis.…”

Section: Introductionmentioning

confidence: 99%