Cancer is one of the major causes of worldwide human mortality. A wide range of cytotoxic drugs are available on the market, and several compounds are in different phases of clinical trials. Many studies suggest that these cytotoxic molecules are also associated with different types of adverse side effects; therefore researchers around the globe are involved in the development of more efficient and safer anticancer drugs. In recent years, quinazoline and its derivatives have been considered as a novel class of cancer chemotherapeutic agents that show promising activity against different tumors. The aim of this article is to comprehensively review and highlight the recent developments concerning the anticancer activity of quinazoline derivatives as well as offer perspectives on the development of novel quinazoline derivatives as anticancer agents in the near future.

An insight into the therapeutic potential of quinazoline derivatives as anticancer agents

Twenty-seven novel (E)-3-[2-arylideneaminoethyl]-2-[4-(trifluoromethoxy)anilino]-4(3H)-quinazolinone derivatives were synthesized by reacting various aromatic aldehydes with intermediate 6. The target compounds were characterized by 1H NMR, 3C NMR, IR, and elemental analysis. Bioassay results revealed that some of the compounds have strong antifungal activities against six fungi (Gibberella zeae, Fusarium oxysporum, Clematis mandshurica, Paralepetopsis sasakii, Phytophthora infestans, and Sclerotinia sclerotiorum) and three bacteria (Xanthomonas oryzae, tomato bacterial wilt, and tobacco bacterial wilt). Notably, these compounds exhibited the highest activity against tomato bacterial wilt and X. oryzae, with 50% effective concentration (EC50) values ranging from 45.96 to 93.31 μg/mL and from 20.09 to 21.33 μg/mL, respectively, which are superior to those of the commercial antibacterial agents thiodiazole-copper (99.80 μg/mL) and bismerthiazol (92.61 μg/mL). These results indicate that novel arylimine deri...

Synthesis and bioactivity evaluation of novel arylimines containing a 3-aminoethyl-2-[(p-trifluoromethoxy)anilino]-4(3H)-quinazolinone moiety.

Discovery of membrane active benzimidazole quinolones-based topoisomerase inhibitors as potential DNA-binding antimicrobial agents

Sulfur and selenium derivatives of quinazoline and pyrido[2,3-d]pyrimidine: Synthesis and study of their potential cytotoxic activity in vitro

Design, synthesis, and antibacterial activity of novel Schiff base derivatives of quinazolin-4(3H)-one.

Synthesis and anti-microbial screening of some Schiff bases of 3-amino-6,8-dibromo-2-phenylquinazolin-4(3H)-ones.

In the present study, a novel schiff bases were synthesized by condensation of 5-subsituted imesatin with different substituted aromatic aldehydes. The chemical structures of the synthesized compounds were confirmed by means of IR, 1H-NMR, 13C-NMR, Mass spectral and Elemental analysis. These synthesized compounds were investigated for analgesic (Tailimmersion method), anti-inflammatory (carrageenan- induced paw oedema method) and antibacterial activities by paper disc diffusion technique. The minimum inhibitory concentrations (MIC) of the compounds were also determined by Agar streak dilution method. Most of the synthesized compounds exhibited significant anti-bacterial and anti-fungal activities. Among the synthesized compounds 5c, 5h, 5i, and 5b exhibited remarkable analgesic and anti-inflammatory activities.

Natesh Ramesh Kumar

Papers

Synthesis and anti-microbial screening of some Schiff bases of 3-amino-6,8-dibromo-2-phenylquinazolin-4(3H)-ones.

Synthesis, analgesic, anti-inflammatory and antimicrobial activities of some novel Schiffâ??s bases of 5-subsituted Isatin

Synthesis and Anti Microbial Studies of Novel 7-(N -4- Substituted Sulfonamide) 6-Fluoroquinolone Derivatives