1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.

Quinoline hybrids and their antiplasmodial and antimalarial activities.

Ciprofloxacin derivatives and their antibacterial activities

Recent advances of pyrazole-containing derivatives as anti-tubercular agents.

4-Quinolone hybrids and their antibacterial activities.

Triazole derivatives and their anti-tubercular activity

Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.

Quinolone derivatives and their activities against methicillin-resistant Staphylococcus aureus (MRSA).

Malaria is a tropical disease, leading to around half a million deaths annually. Antimalarials such as quinolines are crucial to fight against malaria, but malaria control is extremely challenged by the limited pipeline of effective pharmaceuticals against drug-resistant strains of Plasmodium falciparum which are resistant toward almost all currently accessible antimalarials. To tackle the growing resistance, new antimalarial drugs are needed urgently. Hybrid molecules which contain two or more pharmacophores have the potential to overcome the drug resistance, and hybridization of quinoline privileged antimalarial building block with other antimalarial pharmacophores may provide novel molecules with enhanced in vitro and in vivo activity against drug-resistant (including multidrug-resistant) P falciparum. In recent years, numerous of quinoline hybrids were developed, and their activities against a panel of drug-resistant P falciparum strains were screened. Some of quinoline hybrids were found to possess promising in vitro and in vivo potency. This review emphasized quinoline hybrid molecules with potential in vitro antiplasmodial and in vivo antimalarial activity against drug-resistant P falciparum, covering articles published between 2010 and 2019.

Hybrid molecules with potential in vitro antiplasmodial and in vivo antimalarial activity against drug-resistant Plasmodium falciparum.

We report here a concise and divergent enantioselective total synthesis of the revised structures of marine anti-cancer sesquiterpene hydroquinone meroterpenoids (+)-dysiherbols A–E (6–10) using dimethyl predysiherbol 14 as a key common intermediate. Two different improved syntheses of dimethyl predysiherbol 14 were elaborated, one starting from Wieland–Miescher ketone derivative 21, which is regio- and diastereoselectively α-benzylated prior to establishing the 6/6/5/6-fused tetracyclic core structure through intramolecular Heck reaction. The second approach exploits an enantioselective 1,4-addition and a Au-catalyzed double cyclization to build-up the core ring system. (+)-Dysiherbol A (6) was prepared from dimethyl predysiherbol 14via direct cyclization, while (+)-dysiherbol E (10) was synthesized through allylic oxidation and subsequent cyclization of 14. Epoxidation of 14 afforded allylic alcohol 45 or unexpectedly rearranged homoallylic alcohol 44. By inverting the configuration of the hydroxy groups, exploiting a reversible 1,2-methyl shift and selectively trapping one of the intermediate carbenium ions through oxy-cyclization, we succeeded to complete the total synthesis of (+)-dysiherbols B–D (7–9). The total synthesis of (+)-dysiherbols A–E (6–10) was accomplished in a divergent manner starting from dimethyl predysiherbol 14, which led to the revision of their originally proposed structures.

Divergent total synthesis of the revised structures of marine anti-cancer meroterpenoids (+)-dysiherbols A–E

Le Chang

Papers

Triazole derivatives and their anti-tubercular activity

Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.

Quinolone derivatives and their activities against methicillin-resistant Staphylococcus aureus (MRSA).

Hybrid molecules with potential in vitro antiplasmodial and in vivo antimalarial activity against drug-resistant Plasmodium falciparum.

Divergent total synthesis of the revised structures of marine anti-cancer meroterpenoids (+)-dysiherbols A–E