MEDICINAL CHEMISTRY-II

DMCOP
antineoplastic agents

PRANITA JIRVANKAR
(ASSISTANT PROFESSOR)
DEPARTMENT OF PHARMACY
DATTA MEGHE INSTITUTE OF MEDICAL SCIENCES,
DMIMSU (DEEMED UNIVERSITY)
SAWANGI (M) WARDHA
 Purpose statement

DMCOP
At the end of the class the students should be able to, Understand Structure

activity relationship of Antihistaminic drug, and H-1 Antihistaminic drug

 Learning objectives
at the end of the class the students should

S/No Learning objectives Domain Level Criteria Condition

DMCOP
1 Understand Structure activity Cognitive Must know All -
relationship of
Antihistaminic drug.

2 Understand Effect on H-1 Cognitive Must know All -

Antagonist

3 Understand Fate of Cognitive Must know All -

Antihistaminic drugs
4 Understand Effect on other Cognitive Must know All -
receptor
Cancer
• Cancer is characterized by an abnormal and uncontrolled, division of
cells, which produces tumours and invades adjacent normal tissues.

DMCOP
• Antineoplastic agents are drugs used for the treatment of cancer,
malignancy, tumour, carcinoma, sarcoma, leukaemia, or neoplasm
• (Greek neo = new, Plasm = formation).
• Neoplasm refers to a group of diseases caused by several agents,
namely, chemical compounds and radiant energy.
• Cancer is classified into the following categories:
• 1) Carcinoma: This type of cancer starts in the skin or tissues lining the
internal
organs. There are many sub-types of carcinoma, like adenocarcinoma, basal cell
carcinoma, squamous cell carcinoma, and transitional cell carcinoma.

DMCOP
• 2) Sarcoma: This type of cancer starts in the bone, cartilage, fat, muscle, blood
vessels, or other connective or supportive tissues.
• 3) Leukaemia: This type of cancer starts in the blood -forming tissues (i.e., the
bone marrow) and produces numerous abnormal blood cells.
• 4) Lymphoma and Myeloma: This type of cancer starts in the cells of immune
system.
• 5) Central Nervous System Cancers: This type of cancer starts in the brain
and spinal cord tissues.
Antineoplastic or anticancer drugs are
• anticancer drugs are used for treating malignancies or cancerous
growths. Either these drugs are used alone (chemotherapy) or in

DMCOP
• combination with surgery or radiation therapy.
Cell cycle

DMCOP
• Interphase
• Also known as the resting phase of the cell cycle;
• interphase is the time during which the cell prepares for division by
undergoing both cell growth and DNA replication.

DMCOP
• It occupies around 95% time of the overall cycle.
• The interphase is divided into three phases:-
• G1 phase (Gap 1) – G1 phase is the phase of the cell between mitosis
and initiation of replication of the genetic material of the cell. During
this phase, the cell is metabolically active and continues to grow
without replicating its DNA.
• S phase (Synthesis) – DNA replication takes place during this phase.
• If the initial quantity of DNA in the cell is denoted as 2N, then after
replication it becomes 4N.
• However the number of chromosomes does not vary, viz., if the

DMCOP
number of chromosomes during G1 phase was 2n, it will remain 2n at
the end of S phase
• G2­phase (Gap 2) –
• During this phase, the RNA, proteins, other macromolecules required
for multiplication of cell organelles, spindle formation, and cell growth
are produced as the cell prepares to go into the mitotic phase.
M phase
• Mitosis followed by cytokinesis (cell separation)
• Formation of two identical daughter cells
• The mitotic phase is divided into four overlapping stages:-

DMCOP
• Prophase,
• Metaphase,
• Anaphase, and
• Telophase
• G0 phase
• While some cells are constantly dividing, some cell types
are quiescent.
• These cells exit G1 and enter a resting state called G0.
• In G0, a cell is performing its function without actively preparing to

DMCOP
divide.
• G0 is a permanent state for some cells, while others may re-start
division if they get the right signals.
Causes of cancer
• Carcinogenic chemicals and radiations

DMCOP
• Genetic factors
• Life style : diet, smoking, drinking habits .
• Occupational factors : coal tar, mustard gas, chromium, nickel
(employee working in chemical and gas factories .)
• Viruses cause cancer in animals, their role in human cancers has not
been proved
Classification

DMCOP
DMCOP
 Summary

• In this Lecture we was see the Physiological role of Histamine, Types of

histamine receptor, Classification of Antihistaminic.

DMCOP
• We was study the Importance of Structure activity relationship of
Antihistaminic drug.

• We was study the Effect on H-1 Antagonist.

• We was study Fate of Antihistaminic drugs.

• We was study Effect on other receptor

QUESTIONS

DMCOP
 References

1. Kadam, Mahadik, Bothara Principles of Medicinal Chemistry

DMCOP
2. P. Parimoo A Textbook of Medicinal Chemistry

3. John H. Bvlock & John M Wilson , Organic Medicinal & vPharmaceutical

chemistry

4. K.D. Tripathi, Essential of Medical Pharmacology.

DMCOP