Lipophilicity and antiproliferative activity profiling of 2-benzylidencycloalkanones

Analytical tools for the physicochemical profiling of drug candidates to predict absorption/distribution

“…Valko et al also observed linear relationships between log P oct and ϕ 0 , which correspond to the organic modifier concentration (from 0 to 100%) that produces an equimolar distribution between the stationary and mobile phases (i.e., when log k =0) [163,164]. Finally, it should be noted that several linear correlations between log P oct and isocratic log k values at different organic modifier percentages have been described [165][166][167][168][169][170][171][172][173]. However, all these linear relationships are generally better with structurally related compounds (cf., congeneric behavior) or a low number of analytes.…”

Design, synthesis and antiproliferative activity of indole analogues of indanocine

“…Various indanocine analogues have been previously reported, 5,[12][13][14][15][16] however, we wished to apply an approach previously reported by Hudlicky et al in the design of pancratistatin analogue 3 (Fig. 1).…”

“…3. We wished to investigate both the 5membered ring cyclic ketone (4, as found in indanocine 1) and the corresponding 6-membered ring core (5), since indanones 5 and tetralones 14,15,22 of similar compounds were both found to be the most active. In addition, the effects of the N-H hydrogen bonding interaction (R 1 ¼ H, a-d and R 1 ¼ Me, e-h) and various substituted aryl rings (R 2 ¼ Me or OMe and R 3 ¼ H or OH) were also investigated (see Table 1).…”

Synthesis and antifeedant activity of novel alpha-asarone derivatives against stored-product pests

“…In their research, many authors find a line or parabolic relation between biological activity and lipophilicity. In the present study, no simple correlations between specified parameters of lipophilicity and the deterrent activity against the studied species of storage pests were found.…”