[Answer All Parts] [50 Marks] Part (a) The following compound 1 shows anticancer activity through Tankyrase inhibition. Further work led to the development of a 1-D QSAR equation for structure 2 shown below. Question 2 (i) (ii) (iii) OH qa R MeO 1 F 2 Logl/C=0.398 +1.089 +4.541 OH OH Propose a workplan that can be used to identify the pharmacophore for 1 and explain what relevant information will be obtained from each product of your synthetic transformations (detailed synthetic methods are not required). [20 marks] Predict the biological activity for 2 where R = OMe, Br, and NO₂. [10 marks] Structure 3 was identified as the new lead from 3-D QSAR studies. Unfortunately, compound 3 suffered from poor water solubility. Propose a prodrug for 3 that will have enhanced water solubility, include a synthesis for your proposed prodrug and explain how the lead will be released in vivo. [20 marks]

[Answer All Parts] [50 Marks] Part (a) The following compound 1 shows anticancer activity through Tankyrase inhibition. Further work led to the development of a 1-D QSAR equation for structure 2 shown below. Question 2 (i) (ii) (iii) OH qa R MeO 1 F 2 Logl/C=0.398 +1.089 +4.541 OH OH Propose a workplan that can be used to identify the pharmacophore for 1 and explain what relevant information will be obtained from each product of your synthetic transformations (detailed synthetic methods are not required). [20 marks] Predict the biological activity for 2 where R = OMe, Br, and NO₂. [10 marks] Structure 3 was identified as the new lead from 3-D QSAR studies. Unfortunately, compound 3 suffered from poor water solubility. Propose a prodrug for 3 that will have enhanced water solubility, include a synthesis for your proposed prodrug and explain how the lead will be released in vivo. [20 marks]

Chemistry

10th Edition

ISBN:9781305957404

Author:Steven S. Zumdahl, Susan A. Zumdahl, Donald J. DeCoste

Publisher:Steven S. Zumdahl, Susan A. Zumdahl, Donald J. DeCoste

Chapter1: Chemical Foundations

Section: Chapter Questions

Problem 1RQ: Define and explain the differences between the following terms. a. law and theory b. theory and...

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