Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice

Effect of the T-type channel blocker KYS-05090S in mouse models of acute and neuropathic pain

“…KYS-05090S also did not mediate inhibition Nav1.5, nor several types of potassium channels that are expressed in the heart, suggesting that this compound may not have any adverse cardiovascular effects (Table 1). Previously published toxicity tests indicate that this compound is well tolerated at doses up to 26 mg/kg intravenously and 250 mg/kg orally [25] nor was there inhibition of cytochrome P (Lee et al, unpublished results) altogether indicating that this compound may hold further promise for clinical development. Interestingly, KYS-05090S has been shown to have an antitumor activity in vivo in mice [31], which fits with the idea that T-type calcium channels may promote tumor growth [9].…”

T-type Ca2+ Channels: T for Targetable

“…Pioneer studies by Jung and colleagues evaluated the antitumor activity of KYS05090 in a mouse lung adenocarcinoma A549 xenograft, which slowed down tumor growth upon intravenous (61) or oral administration (62). Another 3,4dihydroquinazoline able to block TTCC, KYS05047, demonstrated antitumor efficacy in the same xenograft model when administered orally (63).…”

Quinazolinone and Quinazoline Derivatives: Synthesis and Biological Application

“…A series of novel carbazolyloxy phenylquinazoline derivatives have been developed as angiotensin converting enzyme (ACE) inhibitors. Amongst them compounds (54)(55)(56) showed maximum inhibitory potency in enzyme based assays. The most potent (54-56) compounds have common active site with the Lisinopril binding site [66].…”