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There are so many things for the first-time visitor to see in London, the hardest part is going to be fitting it all in. From all the famous sights that you've heard about for years (Big Ben, Buckingham Palace, etc) to the must-do activities like high tea and shopping at Oxford Street, there's just an overabundance of things to see and do.
Some big ones not to miss:
Buckingham Palace: If the flag is up, that means the Queen is home. You won't be able to go in and have a chat with her, but it's still a pretty cool thing. Although the Palace may be an overrated tourist attraction, if it's your first time here, you really can't see London without a least a cursory stop here. If you want to see the famous changing of the guards, get here early to beat the crowds(especially during the summer months) so you can get a good vantage point. For a first visit may be best to view the outside only but it is possible to view the interior now with conducted tours.
Big Ben and Westminster: probably one of the more photographed architectural sites in London. You've seen it in countless movies ("Look kids, Big Ben") and pictures, now see it for yourself. Walk across the bridge towards the Aquarium to set up and take some fantastic photos. Plus, you get the River Thames (another iconic London symbol) in the shot as well.
Trafalgar Square: once filled with pigeons everywhere you looked, crapping all over the ground and quite possibly the tourists, Trafalgar is a lot more pleasant to visit these days, thanks to a recent law that makes it illegal to feed the flying rats. Climb on up one of the famed Lion statues or climb up the steps to the National Gallery to get a great view of the Square and Big Ben in the distance. The fountains are especially beautiful at nightfall, when the lights below the water illuminate the fountain and water with an ethereal glow.
Piccadilly Circus: A mass of bright lights and neon flashing signs, it's a little like a mini Times Square. The most interesting sight, however, is likely to be the people sitting around the Eros statue in the middle of the square. People with pink mohawks and pierced faces are not an uncommon sight, sitting alongside tourists and locals. From Piccadilly Circus you can walk to Charing Cross, Leicester Square and even Oxford Street (a must-visit location for shopaholics).
London Eye: View the capital city from the heights of the London eye - Views of Big Ben, the Thames, St Paul's and much more, its a certain must-do! Go at dusk and on a nice day see the sunset from the Eye!
The Tower history in spadeloads and the Crown Jewels.
Free culture. the outstanding museums and art galleries. Most provide regular free talks and guided tours.
Bus Tours. there are great many of them. Too many to list here.