OBJECTIVE: To explore an efficient heterocyclic bioisostere as the C3 carboxylic group of antibacterial fluoroquinolones for further development of antitumor fluoroquinolones. METHODS: Using the s-triazole ring as an isosteric replacement of the C3 carboxylic group with another different heterocyclic ring, oxadiazole, as a modified group, new bis-(different azole) methylsulfide derivatives, 6-fluoro-7-(4-methyl-piperazin-1-yl)-1, 8-(2, 1-oxpropyl)-5-[5-(aryl-[1, 3, 4]-oxadiazol-2-methylsulfanyl)-4H-[1, 2, 4]-tri-azol-3yl]-quinolin-4(1H)-ones (6a-6j), were designed from ofloxacin (1). The in vitro antitumor activity of 6a-6j against three cancer cell lines was evaluated by MTT assay. RESULTS: Ten title compounds (6a-6j) ere synthesized and their structures were characterized by spectral data. They exhibited significantly higher in vitro antitumor potency than the parent compound ofloxacin. CONCLUSION: The heterocyclic ring, s-triazole, could be used as an efficient isostere of the C-3 carboxylic group for further development of antitumor fluoroquinolone candidates.

OBJECTIVETo investigate the effect of reconstruction of lower eyelid ectropion with expanded flap.

METHODSFourty patients with lower eyelid ectropion were reconstructed using tissue expander. The volume of the smallest expander was 30 ml, and that of the biggest one was 150 ml. The expand time was from 2-months to 3-months, then advancement or transposition flaps were created and employed in the defected lesion where the scar was removed just in one operation.

RESULTSAll patients have been followed up for 2-year with satisfactory results and no recurrences was appearance.

CONCLUSIONSApplication of expander reasonable may get satisfactory result in reconstruction of lower eyelid ectropion. The incision in donor site is hidden and the symptom seldom recurs.

Adolescent ; Adult ; Blepharoplasty ; methods ; Child ; Ectropion ; surgery ; Humans ; Male ; Surgical Flaps ; Tissue Expansion Devices ; Young Adult